Lumateperone: a new treatment approach for neuropsychiatric disorders.

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Kumar B, Kuhad A, Kuhad A

Lumateperone: a new treatment approach for neuropsychiatric disorders.

Drugs Today (Barc). 2018 Dec;54(12):713-719. doi: 10.1358/dot.2018.54.12.2899443.

PubMed ID

30596390 [ View in PubMed

]

Abstract

Lumateperone tosylate (ITI-007 tosylate, ITI-722) is a first-in-class investigational drug which acts syn-ergistically through multiple systems (serotonergic, dopaminergic and glutamatergic), thus representing a unique approach for the therapeutic management of a range of neuropsychiatric disorders. It possesses a potent antagonistic activity at 5-hydroxytryptamine (serotonin) 2A (5-HT2A) receptors and also binds to dopamine (D1, D2) receptors with partial agonism at presynaptic D2 receptors and postsynaptic antagonism. Further, preclinical data demonstrated that lumateperone uniquely acts as an indirect modulator of glutamatergic phosphoprotein with D1-dependent augmentation of both NMDA and AMPA activity via the mammalian target of rapamycin (mTOR) pathway, mechanisms thought to predict potent and rapid antidepressant effects. Previous results of schizophrenia efficacy studies found robust improvements in depressive as well as psychotic symptoms for those patients who were comorbidly depressed. In various clinical trials to date, the safety profile of lumateperone was found to be similar to that of placebo. These promising results and strong performance in phase II studies point to the potential of lumateperone to display potent and rapid antidepressant effects in patients suffering from a range of mood disorders. Currently, this novel drug is in phase III of its clinical development for schizophrenia, agitation associated with dementia and bipolar depression.

DrugBank Data that Cites this Article

Drugs

Lumateperone

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Lumateperone	5-hydroxytryptamine receptor 2A	Protein	Humans	Yes	Antagonist	Details
Lumateperone	Dopamine D1 receptor	Protein	Humans	Unknown	Not Available	Details
Lumateperone	Dopamine D2 receptor	Protein	Humans	Yes	Partial agonist	Details